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    • 10. 发明申请
    • Asymmetric Synthesis of Rocaglamides via Enantioselective Photocycloaddition Mediated by Chiral Bronsted Acids
    • 通过手性布朗斯台德酸介导的对映选择性光环加成反应的罗卡胶的非对称合成
    • US20090299081A1
    • 2009-12-03
    • US12301727
    • 2007-05-21
    • John A. Porco, JR.Baudouin Gerard
    • John A. Porco, JR.Baudouin Gerard
    • C07D307/77C07D313/06
    • C07D317/12C07D307/93C07D317/72C07D493/08C07D493/10
    • The present invention provides a new strategies for the synthesis of compounds of the rocaglamide family and related natural products. The synthetic approach generally involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by an enantioselective 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile in the presence of a TADDOL derivative. This approach can be used for the formation of adducts containing an aglain core structure. Methods of the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.
    • 本发明提供了合成罗卡酰胺家族化合物和相关天然产物的新策略。 合成方法通常涉及在3-羟基色酮衍生物中光化学生成氧化吡啶鎓物质,随后在TADDOL衍生物存在下,将氧化吡啶类物质的对映选择性1,3-偶极环加成到偶极嗜酸细胞。 该方法可用于形成含有阿格林核心结构的加合物。 还提供了将阿格林核心结构转化为阿格林,罗卡酰胺和巴格林环系统的方法。 本发明还涉及用于制造用于治疗癌症或癌症病症的药物,与细胞过度增殖相关的疾病或NF-κB依赖性病症的药物的罗卡酰胺/阿格林/用于囊霉素衍生物的用途。